Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring matrial. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.
Type:
Grant
Filed:
February 15, 1989
Date of Patent:
October 16, 1990
Assignee:
SRI International
Inventors:
Mitchell A. Avery, Clive Jennings-White
Abstract: Disclosed herein is a novel brassinosteroid derivative represented by the formula: ##STR1## wherein R.sub.3 represents C.sub.1-2 -alkyl,R.sub.1 and R.sub.2 which may be the same or different, represent hydrogen or acyl, respectively, otherwise R.sub.1 and R.sub.2, combining together, may form ##STR2## wherein R.sub.4 and R.sub.5 represent C.sub.1-2 -alkyl, and R.sub.3 represents methyl only in this case.The brassinosteroid derivative represented by the above formula (I) exhibits a favorable plant growth regulating effect on various plants in agriculture and horticulture.
Abstract: This invention relates to (22R,23R,24S)-22,23-epoxy2.alpha.3.alpha.-isopropylidenedioxy-B-homo-7-oxa -5.alpha.-stigmastan-6-one which is of value as a plant growth regulator, a process for preparation thereof and a plant growth regulating composition containing the same.
Abstract: Antiparasitics comprising Avermectin derivatives of formula (I): ##STR1## wherein X represents a single or a double bond; R.sup.1 is H or OH; provided that when X is a single bond, R.sup.1 is H or OH, and when X is a double bond, R.sup.1 is absent;R.sup.2 is an alkyl group substituted by one oxo or one or more hydroxy groups or by a single oxygen atom on two adjacent carbon atoms to form an oxirane ring, or R.sup.2 is an alkyl group substituted by an alkoxycarbonyl group, said substituents on R.sub.2 being attached to either or both a terminal carbon atom and a carbon atom adjacent to a terminal carbon atom of R.sup.2 ; and R.sup.3 is H or CH.sub.3 ; or, when R.sup.2 is oxo-substituted alkyl, an alkyl acetal or ketal derivative thereof.
Abstract: Disclosed herein is a novel steroids represented by the formula (1): ##STR1## wherein Z represents ##STR2## n is integer of 1 to 3, R represents hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy or --CO.sub.2 R', wherein R' represents hydrogen, alkali metal or lower alkyl, andR.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or acyl, respectively.The compound of the formula (1) of the present invention exhibits high durability as well as excellent plant growth regulation.
Abstract: Novel 13-spiro-2'-[tetrahydrofuran]-milbemycins of the formula I ##STR1## in which X represents one of the groups --CH(OR.sub.1)--, --C(.dbd.O)-- or --C(.dbd.N--OH)--;R.sub.1 represents hydrogen or a OH-protecting group;R.sub.2 represents methyl, ethyl, isopropyl or sec.-butyl or the group --C(CH.sub.3).dbd.CH--A in which A represents methyl, ethyl or isopropyl; andR.sub.3 represents hydrogen; C.sub.1 -C.sub.10 -alkyl; C.sub.1 -C.sub.10 -alkyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkoxyalkoxy C.sub.3 -C.sub.9 -alkoxyalkoxyalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.3 -alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, benzyloxy, C.sub.1 -C.sub.6 -acyl and C.sub.1 -C.sub.6 -acyloxy, it being possible for each of the above-mentioned radicals representing or containing an alkoxy group to be terminally substituted at a terminal alkoxy group by hydroxy, halogen, C.sub.1 -C.sub.
Abstract: The invention relates to parasiticidally and insecticidally highly active compounds of formula I ##STR1## wherein R is C.sub.1 -C.sub.10 alkyl;R.sub.1 is hydrogen, a silyl group or a sugar residue; andR.sub.2 is methyl, ethyl, isopropyl or sec-butyl, and to the preparation thereof starting from suitably substituted 15-ester or 13.beta.-ester milbemycins.
Type:
Grant
Filed:
January 17, 1986
Date of Patent:
August 15, 1989
Assignee:
CIBA-GEIGY Corporation
Inventors:
Bruno Frei, Anthony C. O'Sullivan, Jean-Claude Gehret
Abstract: 5-Carbonate derivatives of milbemycins A.sub.3, A.sub.4 and A.sub.5 have valuable acaricidal, anthelmintic and other activities, especially against endo- and exoparasites.
Abstract: Cyclic polyester and especially polyarylate oligomers, typically having degrees of polymerization from 2 to about 7, are prepared by reacting a bisphenol such as bisphenol A or 6,6'-dihydroxy-3,3,3',3'-tetramethylspiro(bis)indane with a dicarboxylic acid chloride such as isophthaloyl or terephthaloyl chloride in the presence of a catalyst, under conditions of low concentration. The cyclic oligomers may be polymerized to linear polyesters by contact with a transesterification catalyst at a temperature in the range of about 200.degree.-300.degree. C.
Abstract: The invention relates to parasiticidally and insecticidally highly active compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a protecting group;R.sub.2 is methyl, ethyl, isopropyl or sec-butyl; andR is a radical R.sub.3 which is bound through oxygen or sulfur and is selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 haloalkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.3 -C.sub.10 alkoxyalkoxyalkyl, hydroxy- or mercapto-substituted C.sub.3 -C.sub.10 alkoxyalkyl, C.sub.4 -C.sub.15 alkoxyalkoxyalkoxyalky, hdroxy- or mercapto-substituted C.sub.4 -C.sub.15 alkoxyalkoxyalkoxyalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 haloalkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.2 -C.sub.10 haloalkynyl, phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.
Abstract: Compounds having the structure: ##STR1## wherein X may be hydrogen, bromine, chlorine, fluorine or iodine are provided, together with methods for synthesizing these compounds, pharmaceutical compositions and use therof for reducing vascular blood flow.Also provided are compounds having the structure: ##STR2## wherein X may be bromine, chlorine, fluorine or iodine, together with methods for preparing the compounds, pharmaceutical compositions and use thereof for reducing vascular blood flow.
Type:
Grant
Filed:
May 30, 1985
Date of Patent:
June 9, 1987
Assignee:
The Trustees of Columbia University in the City of New York
Inventors:
W. Clark Still, Philip R. Hamann, Shripad S. Bhagwat
Abstract: New hexanor-brassinolid-22-ethers are disclosed, of the formula ##STR1## wherein Z is the group ##STR2## OR.sub.2 and OR.sub.3 are oriented cis 2.alpha., 3.alpha. or 2.beta., 3.beta., R.sub.2 and R.sub.3 are the same or different and are each hydrogen formyl, C.sub.2 -C.sub.7 -alkyl-CO--, C.sub.2 -C.sub.7 -alkoxy-C.sub.1 -C.sub.3 -alkyl-CO-- or aryl-CO--, and R.sub.23 is straight-chain or branched C.sub.1 -C.sub.7 -alkyl or C.sub.1 -C.sub.7 -alkoxy-C.sub.1 -C.sub.3 -alkyl. Also disclosed are processes for the production of these compounds as well as compositions containing the same having growth-regulatory activity for plants.
Abstract: Described are compounds of the formula ##STR1## wherein X is hydrogen, loweralkyl, halo, loweralkoxy or trifluoromethyl, and Z is hydrogen, loweralkyl, halo, hydroxy or alkoxy, or compounds of the formula ##STR2## wherein X' and Y' may be the same or different and are selected from hydrogen, loweralkyl, or halo, and Z' is hydrogen, loweralkyl, halo, hydroxy or loweralkoxy, or pharmaceutically acceptable salts thereof.The compounds possess diuretic activity.
Abstract: Novel antibacterially-active analogs of the antibiotics nodusmicin and nargenicin A.sub.1. These compounds are prepared by selectively blocking active hydroxyl groups at the 9, 11 and 18 positions of nodusmicin, and the 11 and 18 positions of nargenicin A.sub.1. Antibacterially-active compounds can be used in various environments to control or eradicate susceptible bacteria. The techniques for such use are well known in the art.
Abstract: New antibacterial tetronolide compounds F-1 and F-2 are produced by fermentation of a microorganism belonging to the genus Micromonospora. The antibiotics F-1 and F-2 are accumulated in the culture liquor and are isolated therefrom respectively and the acyl derivatives of F-1 and F-2, that is, F-1-21-O-acetate, F-1-21-O-propionate, F-1-21-O-n-butylate, F-1 diacetate, F-1 dipropionate, F-2 triacetate, F-2 tripropionate and F-2 tri-n-butylate, etc., are synthesized from F-1 and F-2 by known means.
Abstract: Oxacycloalkenones are prepared by reacting a cycloalkenone with a base in the presence of a dioxygen source in a suitable solvent and isolating the desired product. 1-Hydroxy 2-oxa-3-oxo-.DELTA..sup.4 steroids are convenient synthetic precursors to 2-oxa-3-oxo-.DELTA..sup.4 steroids which find use in modern clinical therapy.